193355-56-5

Upstream product

• 193357-11-8 1-benzyl-4-(4-fluorobenzyl)-4-hydroxypiperidine 
• 3612-20-2 1-phenylmethyl-4-piperidone 
• 352-11-4 1-chloromethyl-4-fluorobenzene 
• 942997-83-3 4-(4-fluoro-benzyl)-4-hydroxy-piperidine-1-carboxylic acid benzyl ester 
• 1643-73-8 (4-fluorobenzyl)magnesium chloride 
• 309915-33-1 tert-butyl 4-(4-fluorobenzyl)-4-hydroxypiperidine-1-carboxylate 
• 79099-07-3 N-tert-butyloxycarbonylpiperidin-4-one 

Downstream Products

• 193357-76-5 1-[2-(4-benzyloxyphenoxy)ethyl]-4-(4-fluorobenzyl)-4-hydroxypiperidine 
• 231947-14-1 4-(4-fluorobenzyl)-1-but-3-ynyl-4-hydroxypiperidine 
• 302800-02-8 4-(4-fluoro-benzyl)-1-prop-2-ynyl-piperidin-4-ol 
• 333988-96-8 1-Acetyl-N-(3-chlorophenyl)-N-{3-[4-(4-fluorobenzyl)-4-hydroxy-1-piperidinyl]propyl}-4-piperidinecarboxamide 

Relevant academic research and scientific papers

Synthesis and SAR of thieno[3,2-b]pyridinyl urea derivatives as urotensin-II receptor antagonists

The preparation and SAR profile of thieno[3,2-b]pyridinyl urea derivatives as novel and potent urotensin-II receptor antagonists are described. An activity optimization study, probing the effects of substituents on thieno[3,2-b]pyridinyl core and benzyl group of the piperidinyl moiety, led to the identification of p-fluorobenzyl substituted thieno[3,2-b]pyridinyl urea 6n as a highly potent UT antagonist with an IC50 value of 13 nM. Although 6n displays good metabolic stability and low hERG binding activity, it has an unacceptable oral bioavailability.

MONOCYCLIC AND BICYCLIC COMPOUNDS AND METHODS OF USE

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

INHIBITORS OF TRYPTASE

The present invention related to certain inhibitors of tryptase that are inhibitors of tryptase, pharmaceutical composition comprising these compounds and method of treating asthma, allergic rhinitis, and/or Chronic Obstructive Pulmonary Disease utilizing these compounds.

PIPERIDINE DERIVATIVES AS ANTAGONISTS OF THE CC CHEMOKINE RECEPTOR CCR1 AND THEIR USE AS ANTI-INFLAMMATORY AGENTS

Piperidine derivatives of the following formulae (I) and (II) and their pharmaceutically acceptable salts, which are functional antagonists of the CC chemokine receptor CCR1 and are thus useful as anti inflammatory agents, a pharmaceutical compositions co

INDOLE DERIVATIVE AND USE FOR TREATMENT OF CANCER

The present invention relates to a compound represented by the formula (I’) wherein A is a benzene ring optionally having substituents, R1, R2a and R3 are each a hydrogen atom, a hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, R1 and R2a may form a ring via X, when R1 and R2a form a ring via X, R1 and R2a are each a bond or a divalent C1-5 acyclic hydrocarbon group optionally having substituents, and X is a bond, an oxygen atom, an optionally oxidized sulfur atom or an imino group optionally having a substituent, provided that R1, R2a and X are not bonds at the same time, or a salt thereof, and an agent for inhibiting kinase (phosphorylation enzyme), which contains this compound or a prodrug thereof. The compound of the present invention has an inhibitory activity against kinase such as a vascular endothelial growth factor receptor (VEGFR) and the like, and is useful as an agent for the prophylaxis or threatment of cancer and the like.

4-substituted piperidine analogs and their use as subtype selective NMDA receptor antagonists

PCT No. PCT/US96/20872 Sec. 371 Date Sep. 16, 1998 Sec. 102(e) Date Sep. 16, 1998 PCT Filed Dec. 20, 1996 PCT Pub. No. WO97/23216 PCT Pub. Date Jul. 3, 1997Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs are selective active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, psychosis, anxiety, migraine headaches, glaucoma, CMV retinitis, aminoglycoside antibiotics-induced hearing loss, convulsions, chronic pain, opioid tolerance or withdrawal, urinary incontinence or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.

4-HYDROXY-PIPERODINE DERIVATIVES

The present invention relates to compounds of the formula STR1 wherein x is--O--,--NH--,--CH 2--,--CH=,--CO 2--,--CONH--,--CON(lower alkyl)--,--S--and--SO 2--; R. sup.1-R. sup.4 are, independently from each other hydrogen, halogen, hydroxy, amino, nitro, lower-alkyl-sulfonylamido, 1-or 2-imidazolyl, 1-(1,2,4-triazolyl) or acetamido;R 5, R 6 are, independently from each other hydrogen, lower-alkyl, hydroxy, lower alkoxy or oxo;R. sup.7-R 10 are, independently from each other hydrogen, lower-alkyl, halogen, trifluoromethyl or lower-alkoxy;n is 0 or 1; and to pharmaceutically acceptable acid addition salts thereof. Compounds of the present invention are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers.

Subtype-selective N-methyl-D-aspartate receptor antagonists: Synthesis and biological evaluation of 1-(arylalkynyl)-4-benzylpiperidines

A search of our compound library for compounds with structural similarity to ifenprodil (5) and haloperidol (7) followed by in vitro screening revealed that 4-benzyl-1-(4-phenyl-3-butynyl)piperidine (8) was a moderately potent and selective antagonist of the NR1A/2B subtype of NMDA receptors. Substitution on the benzyl group of 8 did not significantly affect NR1A/2B potency, while addition of hydrogen bond donors in the para position of the phenyl group enhanced NR1A/2B potency. Addition of a hydroxyl moiety to the 4-position of the piperidine group slightly reduced NR1A/2B potency while reducing α-1 adrenergic and dopamine D2 receptor binding affinities substantially, resulting in improved overall selectivity for NR1A/2B receptors. Finally, the butynyl linker was replaced with propynyl or pentynyl. When the phenyl was para substituted with amine or acetamide groups, the NR1A/2B potency order was butynyl > pentynyl >> propynyl. For the para methanesulfonamide or hydroxyl groups, the order was butynyl ? propynyl > pentynyl. The hydroxyl propyne (48) and butyne (23) were among the most potent NR1A/2B antagonists from this study. They both potentiated the effects of L-DOPA in the 6-hydroxydopamine-lesioned rat, a model of Parkinson's disease, dosed at 10 mg/kg ip, but 48 was not active at 30 mg/kg po.